公开(公告)号：US20240358703A1

公开(公告)日：2024-10-31

申请号：US18418061

申请日：2024-01-19

申请人： KURA ONCOLOGY, INC.

发明人： Francis BURROWS ,  Linda V. KESSLER ,  Liansheng LI ,  Pingda REN ,  Yi WANG ,  Tao WU ,  Jingchuan ZHANG

IPC分类号： A61K31/519 ,  A61K31/44 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/505 ,  A61K31/5377 ,  A61P35/02

CPC分类号： A61K31/519 ,  A61K31/44 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/505 ,  A61K31/5377 ,  A61P35/02

摘要： The present disclosure provides methods for treating hematological malignancies and Ewing's sarcoma using menin inhibitors. Compositions for use in these methods are also provided.

公开(公告)号：US12128111B2

公开(公告)日：2024-10-29

申请号：US17345582

申请日：2021-06-11

申请人： Jiangnan University

发明人： Jing Hu ,  Jian Yin ,  Jun Hu

IPC分类号： C07H1/00 ,  A61K31/44 ,  A61K31/513 ,  A61K31/704 ,  A61K41/00 ,  A61K47/54 ,  A61K47/60 ,  A61K47/69

CPC分类号： A61K47/6949 ,  A61K31/44 ,  A61K31/513 ,  A61K31/704 ,  A61K41/0071 ,  A61K47/546 ,  A61K47/549 ,  A61K47/60 ,  C07H1/00

摘要： The disclosure discloses a glyco-metal-organic frameworks-based hepatic targeted therapeutic drug and a preparation method thereof, and belongs to the field of biomedicine. The disclosure loads a chemotherapeutic drug onto specific metal-organic frameworks, and modifies targeted molecule galactose on the surface of the materials through amide reaction. The biocompatibility and cytotoxicity of the obtained hepatic targeted therapeutic drug have been carefully evaluated at the cellular level. The hepatic targeted therapeutic drug of the disclosure has good stability and acidic pH triggered drug release property, and can exert the synergistic therapeutic effect of photodynamic therapy and chemotherapy. In addition, in vivo behavioral tracing and therapeutic efficacy are evaluated in mouse models with subcutaneous solid tumor and tumor in situ, and the disclosure is expected to play a huge role in clinical applications.

公开(公告)号：US12128014B2

公开(公告)日：2024-10-29

申请号：US17711572

申请日：2022-04-01

申请人： MERCAPTOR DISCOVERIES, INC.

发明人： Todd C. Zankel ,  Sara Louise Isbell

IPC分类号： A61K31/145 ,  A61K31/095 ,  A61K31/198 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/407 ,  A61K31/415 ,  A61K31/44 ,  A61K31/445 ,  A61K31/506 ,  A61P25/08

CPC分类号： A61K31/145 ,  A61K31/095 ,  A61K31/198 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/407 ,  A61K31/415 ,  A61K31/44 ,  A61K31/445 ,  A61K31/506 ,  A61P25/08

摘要： The present disclosure relates, in general, to use of small diffusible thiols in the treatment of neurodegenerative diseases associated with glutamate excitotoxicity, protein aggregation and oxidative stress in the central nervous system, particularly in the brain.

公开(公告)号：US20240350432A1

公开(公告)日：2024-10-24

申请号：US18640714

申请日：2024-04-19

申请人： Bobbi Jo Mullins ,  University of Kentucky Research Foundation

发明人： Jill Rebecca Turner Ortinski ,  Linda P. Dwoskin ,  Bobbie Jo Mullins

IPC分类号： A61K31/13 ,  A61K9/00 ,  A61K31/44 ,  A61K31/465 ,  A61K31/573 ,  A61K45/06 ,  A61P31/12

CPC分类号： A61K31/13 ,  A61K9/0019 ,  A61K31/44 ,  A61K31/465 ,  A61K31/573 ,  A61K45/06 ,  A61P31/12

摘要： This disclosure relates to methods for the prevention and/or treatment of neurological adverse effects caused by viral infections in a subject. In some aspects, the methods include administration of at least one N-methyl-D-aspartic acid receptor (NMDAR) antagonist to a subject as a preventative treatment. In other aspects, the NMDAR antagonists may be used as a treatment following a viral infection or suspected viral infection.

公开(公告)号：US12110263B2

公开(公告)日：2024-10-08

申请号：US17740260

申请日：2022-05-09

申请人： CORTEXYME, INC.

发明人： Andrei W. Konradi ,  Robert A. Galemmo, Jr. ,  Stephen S. Dominy ,  Casey C. Lynch ,  Leslie J. Holsinger

IPC分类号： C07C233/62 ,  A61K31/165 ,  A61K31/167 ,  A61K31/41 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/513 ,  A61K31/655 ,  A61K45/06 ,  A61P25/00 ,  A61P31/04 ,  C07B59/00 ,  C07C233/78 ,  C07C235/10 ,  C07C235/50 ,  C07C237/42 ,  C07C245/08 ,  C07C247/16 ,  C07C247/18 ,  C07C317/28 ,  C07C323/40 ,  C07C323/42 ,  C07C381/00 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D213/81 ,  C07D213/82 ,  C07D239/34 ,  C07D239/36 ,  C07D239/38 ,  C07D257/04 ,  C07D261/12 ,  C07D401/12 ,  C07D413/12 ,  C07F5/02

CPC分类号： C07C233/62 ,  A61K31/165 ,  A61K31/167 ,  A61K31/41 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/513 ,  A61K31/655 ,  A61K45/06 ,  A61P25/00 ,  A61P31/04 ,  C07B59/001 ,  C07C233/78 ,  C07C235/10 ,  C07C235/50 ,  C07C237/42 ,  C07C245/08 ,  C07C247/16 ,  C07C247/18 ,  C07C317/28 ,  C07C323/40 ,  C07C323/42 ,  C07C381/00 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D213/81 ,  C07D213/82 ,  C07D239/34 ,  C07D239/36 ,  C07D239/38 ,  C07D257/04 ,  C07D261/12 ,  C07D401/12 ,  C07D413/12 ,  C07F5/02 ,  C07C2601/08

摘要： The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.

公开(公告)号：US12109201B2

公开(公告)日：2024-10-08

申请号：US17843028

申请日：2022-06-17

申请人： Ovid Therapeutics, Inc.

发明人： Matthew During

IPC分类号： A61K31/437 ,  A61K9/00 ,  A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/197 ,  A61K31/27 ,  A61K31/325 ,  A61K31/36 ,  A61K31/4015 ,  A61K31/4166 ,  A61K31/4192 ,  A61K31/423 ,  A61K31/433 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4535 ,  A61K31/513 ,  A61K31/515 ,  A61K31/53 ,  A61K31/55 ,  A61K31/5513 ,  A61K31/5517 ,  A61K31/57 ,  A61K31/7048 ,  A61K45/06

CPC分类号： A61K31/437 ,  A61K9/0019 ,  A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/197 ,  A61K31/27 ,  A61K31/325 ,  A61K31/36 ,  A61K31/4015 ,  A61K31/4166 ,  A61K31/4192 ,  A61K31/423 ,  A61K31/433 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4535 ,  A61K31/513 ,  A61K31/515 ,  A61K31/53 ,  A61K31/55 ,  A61K31/5513 ,  A61K31/5517 ,  A61K31/57 ,  A61K31/7048 ,  A61K45/06 ,  A61K31/437 ,  A61K2300/00 ,  A61K31/57 ,  A61K2300/00 ,  A61K31/5517 ,  A61K2300/00 ,  A61K31/5513 ,  A61K2300/00 ,  A61K31/44 ,  A61K31/04 ,  A61K2300/00 ,  A61K2300/00 ,  A61K31/27 ,  A61K2300/00 ,  A61K31/433 ,  A61K2300/00 ,  A61K31/55 ,  A61K2300/00 ,  A61K31/4015 ,  A61K2300/00 ,  A61K31/195 ,  A61K2300/00 ,  A61K31/165 ,  A61K2300/00 ,  A61K31/53 ,  A61K2300/00 ,  A61K31/444 ,  A61K2300/00 ,  A61K31/515 ,  A61K2300/00 ,  A61K31/4166 ,  A61K2300/00 ,  A61K31/4192 ,  A61K2300/00 ,  A61K31/19 ,  A61K2300/00 ,  A61K31/513 ,  A61K2300/00 ,  A61K31/36 ,  A61K2300/00 ,  A61K31/4535 ,  A61K2300/00 ,  A61K31/7048 ,  A61K2300/00 ,  A61K31/197 ,  A61K2300/00 ,  A61K31/423 ,  A61K2300/00 ,  A61K31/136 ,  A61K2300/00

摘要： Use of allosteric modulators and/or gaboxadol for the treatment of epileptic disorders in a subject in need thereof.

公开(公告)号：US20240325359A1

公开(公告)日：2024-10-03

申请号：US18599793

申请日：2024-03-08

申请人： Trustees of Dartmouth College

发明人： Ta Yuan CHANG ,  Catherine C.Y. CHANG ,  Adrianna DE LA TORRE

IPC分类号： A61K31/44 ,  A61K9/51 ,  C07D213/75

CPC分类号： A61K31/44 ,  A61K9/5123 ,  C07D213/75

摘要： A high potency, brain-permeable compound that inhibits Acyl-CoA:Cholesterol Acyltransferase 1 (ACAT1) activity is provided as are pharmaceutical compositions and methods for treating a disease, disorder, or condition mediated by ACAT1.

公开(公告)号：US20240325354A1

公开(公告)日：2024-10-03

申请号：US18735806

申请日：2024-06-06

申请人： Alzheon, Inc.

发明人： Petr Kocis ,  Martin Tolar ,  John Hey

IPC分类号： A61K31/4196 ,  A61K31/426 ,  A61K31/433 ,  A61K31/44 ,  A61K31/505 ,  A61P25/28

CPC分类号： A61K31/4196 ,  A61K31/426 ,  A61K31/433 ,  A61K31/44 ,  A61K31/505 ,  A61P25/28

摘要： Methods of treating a disease characterized by amyloid aggregates are provided herein.

公开(公告)号：US20240317708A1

公开(公告)日：2024-09-26

申请号：US18573802

申请日：2022-06-30

申请人： ZEDIRA GMBH

发明人： Ralf PASTERNACK ,  Christian BÜCHOLD ,  Martin HILS ,  Martin STIELER ,  Uwe GERLACH

IPC分类号： C07D401/12 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4748 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  C07D213/75 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

CPC分类号： C07D401/12 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4748 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  C07D213/75 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

摘要： The invention relates to the compound of general formula (I) as novel inhibitors of transglutaminases, to methods for producing the inventive compounds, to pharmaceutical compositions containing said inventive compounds and to their use for the prophylaxis and treatment of diseases associated with transglutaminases, in particular transglutaminase 2.

公开(公告)号：US20240295545A1

公开(公告)日：2024-09-05

申请号：US18276956

申请日：2022-02-11

申请人： Imperial College Innovations Limited

发明人： Valentin K. Gribkoff ,  Kambiz N. Alavian ,  Travis S. Tierney

IPC分类号： G01N33/50 ,  A61K31/075 ,  A61K31/381 ,  A61K31/423 ,  A61K31/426 ,  A61K31/44 ,  A61K31/495 ,  A61P35/00 ,  G01N21/64

CPC分类号： G01N33/5079 ,  A61K31/075 ,  A61K31/381 ,  A61K31/423 ,  A61K31/426 ,  A61K31/44 ,  A61K31/495 ,  A61P35/00 ,  G01N21/6428 ,  G01N33/5058 ,  G01N2500/10

摘要： The invention is directed to a method for identifying a candidate anti-glioma drug that is a mitochondrial F1Fo ATP Synthase c-subunit leak channel opener, the method comprising: a. providing an admixture comprising: i. a candidate drug; ii. a submitochondrial vesicle (SMV) preparation; and iii. an H+ probe, wherein the H+ probe remains outside of the SMV(s); b. contacting the admixture with ATP; c. measuring a level of H+ outside of the SMV(s) via the H+ probe; d. comparing the level of H+ at step c) with a level of H+ in a control admixture lacking the candidate drug; and identifying the drug as a candidate anti-glioma drug that is a mitochondrial F1Fo ATP Synthase c-subunit leak channel opener, when the level of H+ is higher compared to the level of H+ in the control admixture; or identifying that the drug is not a candidate anti-glioma drug that is a mitochondrial F1Fo ATP Synthase c-subunit leak channel opener, when the level of H+ is the same or lower compared to the level of H+ in the control admixture.